Rp-8-pCPT-Cyclic GMPS (sodium salt)

IC50: 18.3 and 0.16 μM for cGK Iα and cGK II, respectively. Rp-8-pCPT-Cyclic GMPS is a GMP-dependent protein kinases (cGKs) inhibitor. Appreciation of cGMP as a distinct intracellular second messenger is reported to be closely followed by an intensive search for effector proteins in various organisms. A cGMP-dependent protein kinase (cGK) has been found in arthropods resulting in the eventual isolation of cGK from mammalian tissues. In vitro: Previous study found that Rp-8-pCPT-Cyclic GMPS could selectively inhibit cGK activity in intact human platelets. The IC50 value of Rp-8-pCPT-Cyclic GMPS for cGK II was 114-fold lower than that for cGK Iα in the presence of 1 mM cGMP. In the presence of 10 mM cGMP, the IC50 values of Rp-8-pCPT-Cyclic GMPS for cGK Iα and cGK II increased 3- and 11-fold, respectively. In addition, millimolar concentrations of Rp-8-pCPT-Cyclic GMPS could fully activate both enzymes, a phenomenon that was observed previously for cGK II. Because substitutions at the 8-position of the guanine ring are poorly tolerated by cGK Ib, these results suggested that the Rp-isomer of 8-pCPT-cGMPS might be a selective activator or inhibitor, respectively, of cGK II compared to the cGK I isoforms . In vivo: Up to now, there is no animal in vivo study reported. Clinical trial: So far, no clinical study has been conducted.

Product information

CAS Number: 208445-07-2

Molecular Weight: 525.86

Formula: C16H14ClN5NaO6PS2

Chemical Name: sodium [(2R,4aR,6R,7R,7aS)-6-{2-amino-8-[(4-chlorophenyl)sulfanyl]-6-oxo-6,9-dihydro-1H-purin-9-yl}-7-hydroxy-2-oxo-hexahydro-2λ⁵-furo[3,2-d][1,3,2]dioxaphosphinin-2-yl]sulfanide

Smiles: [Na+].NC1NC(=O)C2N=C(SC3C=CC(Cl)=CC=3)N([C@@H]3O[C@@H]4CO[P@@](=O)([S-])O[C@H]4[C@H]3O)C=2N=1

InChiKey: JERAACMSJYSCBY-TXBWCVORSA-M

InChi: InChI=1S/C16H15ClN5O6PS2.Na/c17-6-1-3-7(4-2-6)31-16-19-9-12(20-15(18)21-13(9)24)22(16)14-10(23)11-8(27-14)5-26-29(25,30)28-11;/h1-4,8,10-11,14,23H,5H2,(H,25,30)(H3,18,20,21,24);/q;+1/p-1/t8-,10-,11-,14-,29-;/m1./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.